PXS-4787 是一种特异、有效的泛赖氨酸氧化酶 (lysyl oxidase) 抑制剂，能够消除赖氨酸氧化酶活性。PXS-4787 抑制LOX的IC50分别为 2 μM (Bovine LOX)，3.2 μM (rh LOXL1)，0.6 μM (rh LOXL2)，1.4 μM (rh LOXL3)，0.2 μM (rh LOXL4)。
| 生物活性 | PXS-4787 is a specific and effective pan-LOX(lysyl oxidase) inhibitor for abolishing lysyl oxidase activity. PXS-4787 inhibitsLOXwithIC50s of 2 μM (Bovine LOX), 3.2 μM (rh LOXL1), 0.6 μM (rh LOXL2), 1.4 μM (rh LOXL3), 0.2 μM (rh LOXL4), respectively[1]. |
| IC50& Target | 2 μM (Bovine LOX), 3.2 μM (rh LOXL1), 0.6 μM (rh LOXL2), 1.4 μM (rh LOXL3), 0.2 μM (rh LOXL4)[1] |
体外研究
(In Vitro) | Lysyl oxidases stabilize the main component of scar tissue, collagen, and drive scar stiffness and appearance[1].
PXS-4787 (0-10 μM; 15 min-4 h) dose- and time-dependently inhibits lysyl oxidase and displays comparable inhibitory activity across species[1].
PXS-4787 (0-100 μM; 72 h) is well tolerated by primary human dermal fibroblasts, (10 μM; 11 d) reduces collagen formation, deposition and crosslinking in primary human dermal fibroblasts cultured in vitro[1].
PXS-4787 (10 μM; 48 h) induces differential gene expression in fibroblasts and keratinocytes, including COL1A1, LOX, GAPDH, PGK1[1].
Immunofluorescence[1] | Cell Line: | Primary human dermal fibroblasts cultured in vitro | | Concentration: | 0, 1, 10 μM | | Incubation Time: | 11 days | | Result: | Significantly reduced in the 10 μM treatment group. |
RT-PCR[1] | Cell Line: | Cultured fibroblasts and keratinocytes (isolated from five different patients) | | Concentration: | 10 μM | | Incubation Time: | 48 hours | | Result: | Resulted four genes with significant differential expression in fibroblasts and two differentially expressed genes in keratinocytes. |
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体内研究
(In Vivo) | PXS-4787 (3%, oil in water cream; external application; once daily, for 28 days) reduces collagen deposition and cross-linkin in murine models of injury and fibrosis under topical application[1].
PXS-4787 (3%, oil in water cream; external application; once daily, for 12 weeks) also significantly improves scar appearance without reducing tissue strength in porcine injury models under topical application[1].
| Animal Model: | Porcine excision injury model (female Juvenile pigs, 18-20 kg)[1] | | Dosage: | 3%, oil in water cream; 400 mg cream applied to 16 cm2 | | Administration: | External application; 1, 2 and 3 weeks post-injury; once dailly, for 12 weeks | | Result: | Improved the appearance of scar in relevant in vivo models, indicative of a targetdriven, as opposed to compound-specific, effect. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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